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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Journal of neural transmission 103 (1996), S. 1153-1161 
    ISSN: 1435-1463
    Keywords: Sigma receptors ; neck dystonia ; red nucleus ; BMY-14802 ; neuroleptics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary To clarify clinical roles of σ receptor binding affinity of neuroleptics, neck dystonia induced by microinjection of σ receptor ligands and neuroleptics into rat red nucleus was investigated. DTG and (+)-3-PPP, putative σ receptor agonists, induced neck dystonia in dose-dependent and reversible manner. Haloperidol and perphenazine induced dystonia in the same way as σ receptor agonists, whereas zotepine and (−)-sulpiride did not. The rank order of potency in induction of dystonia and σ receptor affinity of these compounds showed positive correlation. Although BMY-14802 has a high affinity for σ receptors, it never produced dystonia by itself. On the other hand, combined injection of BMY-14802 with DTG attenuated DTG-induced dystonia. Therefore, it is suggested that typical neuroleptics such as haloperidol act agonistic and atypical neuroleptics such as BMY-14802 act antagonistic at rubral σ receptors in the induction of neck dystonia.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1435-1463
    Keywords: Sigma receptors ; (+)-3PPP ; BMY-14802 ; in vivo microdialysis ; dopamine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Intraperitoneal injection of (+)-3-[3-hydroxyphenyl)-N-(1-propyl)piperidine ((+)-3PPP), a sigma receptor agonist, significantly reduced the striatal levels of dopamine (DA), 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) measured by in vivo microdialysis. These reductions were significantly greater at (+)-3PPP doses of 12 and 24 mg/kg than at 1 mg/ kg. The levels of 5-hydroxyindoleacetic acid (5HIAA) were increased by the injection of (+)-3PPP in dose of 24 mg/kg, but were not affected at lower doses. BMY-14802, a sigma antagonist, alone at doses of 15 mg/kg and 30 mg/kg did not affect the levels of DA, DOPAC, HVA and 5HIAA. Pretreatment with 30 mg/kg BMY-14802 reversed the reduction of the levels of DA induced by 12 mg/kg (+)-3PPP. Although neither 30 mg/kg BMY-14802 nor 12 mg/kg (+)-3PPP affected the levels of striatal 5HIAA, combined treatment with both produced a significant elevation. These findings clearly demonstrate that sigma receptors may regulate DA release from the striatal presynapse.
    Type of Medium: Electronic Resource
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